氨基倍半萜内酯作为新型抗白血病药物：NF-κB抑制剂DMAPT（LC-1）的发现。
Aminoparthenolides as novel anti-leukemic agents: Discovery of the NF-kappaB inhibitor, DMAPT (LC-1).
作者信息
Neelakantan Sundar, Nasim Shama, Guzman Monica L, Jordan Craig T, Crooks Peter A
机构信息
Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536, USA.
出版信息
Bioorg Med Chem Lett. 2009 Aug 1;19(15):4346-9. doi: 10.1016/j.bmcl.2009.05.092. Epub 2009 May 27.
A series of aminoparthenolide analogs (6-37) were synthesized and evaluated for their anti-leukemic activity. Eight compounds exhibited good anti-leukemic activity with LD(50)'s in the low microM range (1.5-3.0microM). Compounds 16, 24 and 30 were the most potent compounds in the series, causing greater than 90% cell death at 10microM concentration against primary AML cells in culture, with LD(50) values of 1.7, 1.8 and 1.6microM.
合成了一系列青蒿素甲醚类似物（6 - 37），并对其抗白血病活性进行了评估。八种化合物表现出良好的抗白血病活性，半数致死剂量（LD(50)）在低 microM 范围内（1.5 - 3.0 microM）。化合物 16、24 和 30 是该系列中最有效的化合物，在 10 microM 浓度下对培养的原发性 AML 细胞导致超过 90% 的细胞死亡，其 LD(50) 值分别为 1.7、1.8 和 1.6 microM。
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